A CONTINUOUS FLOW PROCESS FOR THE PREPARATION OF INGENOL-3-MEBUTATE
    1.
    发明申请
    A CONTINUOUS FLOW PROCESS FOR THE PREPARATION OF INGENOL-3-MEBUTATE 审中-公开
    用于制备INGENOL-3-MEBUTATE的连续流程

    公开(公告)号:WO2015176175A1

    公开(公告)日:2015-11-26

    申请号:PCT/CA2015/050300

    申请日:2015-04-10

    摘要: Disclosed is a continuous process for the preparation of ingenol-3-mebutate by reaction, in solution, of ingenol or ingenol anion and angelic anhydride or an equivalent angelylating agent. The continuous flow process is preferably performed in the presence of a base such as lithium hexamethyl disilazane (LiHMDS) and/or an activating agent such as dicyclohexylcarbodiimide (DCC). Also disclosed is a process for recycling the other reaction products obtained in the continuous process for preparation of ingenol-3-mebutate for formation of ingenol, which can then be recycled to form ingenol-3-mebutate.

    摘要翻译: 公开了通过在溶液中,在溶液中,通过在溶液中制备烯内酰脲-3-甲酸酯的连续方法,所述方法包括将所述烯醇化合物或游离酸酐或邻苯二甲酸酐或当量的酰胺化剂反应。 连续流动方法优选在诸如六甲基二硅氮烷锂(LiHMDS)和/或活化剂如二环己基碳二亚胺(DCC)的碱的存在下进行。 还公开了一种用于回收在连续制备用于形成烯内酯的烯醇酚-3-甲酸酯的连续方法中获得的其它反应产物的方法,然后可以将其再循环以形成烯醇酚-3-甲酸酯。